Tirofiban
- Atc Codes:B01AC17
- CAS Codes:150915-40-5#142373-60-2#144494-65-5
- PHARMGKB ID:150915-40-5#142373-60-2#144494-65-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Aggrastat; Belgium: Aggrastat; Estonia: Aggrastat; Finland: Aggrastat; France: Agrastat; Germany: Aggrastat; Greece: Aggrastat; Hungary: Aggrastat; Ireland: Aggrastat; Italy: Aggrastat; Latvia: Aggrastat; Lithuania: Aggrastat; Malta: Aggrastat; Netherlands: Aggrastat; Poland: Aggrastat; Portugal: Aggrastat; Romania: Aggrastat; Spain: Agrastat; Sweden: Aggrastat; UK: Aggrastat.
North America
Canada: Aggrastat; USA: Aggrastat.
Latin America
Argentina: Agrastat; Brazil: Agrastat; Mexico: Agrastat.
Drug combinations
Chemistry
Tirofiban Hydrochloride: C~22~H~36~N~2~O~5~S HCl H~2~O. Mw: 495.07. (1) L-Tyrosine, N-(butylsulfonyl)-O-[4-(4-piperidinyl)butyl]-, monohydrochloride, monohydrate; (2) N-(Butylsulfonyl)-4-[4-(4-piperidyl)butoxy]-L-phenylalanine monohydrochloride monohydrate. CAS-150915-40-5; CAS-142373-60-2 (anhydrous); CAS-144494-65-5 (tirofiban)(1994).
Pharmacologic Category
Antithrombotic Agents; Platelet-aggregation Inhibitors; Glycoprotein IIb/IIIa Inhibitor. (ATC-Code: B01AC17).
Mechanism of action
A reversible antagonist of fibrinogen binding to GPIIb/IIIa receptor. When administered intravenously, inhibits ex vivo platelet aggregation. When given according to recommended regimen, >90% inhibition attained by the end of the 30-minute infusion. Platelet aggregation inhibition is reversible following cessation of the infusion.
Therapeutic use
Indicated, in combination with heparin, for treatment of acute coronary syndrome, including patients who are to be managed medically and those undergoing PTCA or atherectomy. In this setting, it has been shown to decrease rate of combined endpoint of death, new myocardial infarction or refractory ischemia/repeat cardiac procedure.
Pregnancy and lactiation implications
Use with caution in pregnant women. Excretion in breast milk unknown (contraindicated in nursing women).
Unlabeled use
Contraindications
Hypersensitivity to tirofiban or any component of the formulation. Active internal bleeding or history of bleeding diathesis within previous 30 days. History of intracranial hemorrhage, intracranial neoplasm, arteriovenous malformation, or aneurysm. History of thrombocytopenia following prior exposure. History of CVA within 30 days or any history of hemorrhagic stroke. Major surgical procedure or severe physical trauma within previous month. History, symptoms, or findings suggestive of aortic dissection. Severe hypertension. Concomitant use of another parenteral GP IIb/IIIa inhibitor. Acute pericarditis.
Warnings and precautions
Bleeding common, including retroperitoneal, pulmonary, and spontaneous GI and/or GU bleeding. Use with extreme caution in platelet counts <150000/mm^3^, hemorrhagic retinopathy, previous history of GI disease, recent thrombolytic therapy and in chronic dialysis. Use caution with administration of other drugs affecting hemostasis. Adjust dose with severe renal dysfunction (CrCl <30 mL/minute). Prior to pulling sheath, heparin should be discontinued for 3-4 hours and ACT <180 seconds or APTT <45 seconds.